Recent advances in drug delivery and formulation最新文献

Introduction: This study focused on creating an innovative treatment approach for Parkinson's disease (PD), a progressive neurodegenerative condition characterized by the loss of specific neurons in the brain.

Aim: The research aimed to develop a nasal gel using gellan gum containing a complex of chrysin with hydroxypropyl-β-cyclodextrin (HP-β-CD) to enhance the drug's solubility and stability.

Method: The formulation process involved utilizing central composite design (CCD) to optimize the concentrations of gellan gum and HPMC E5, with viscosity and mucoadhesive strength as key factors. The resulting optimized In Situ gel comprised 0.7% w/v gellan gum and 0.6% w/v HPMC E5, exhibiting desirable viscosity levels for both sol and gel states, along with robust mucoadhesive properties. The formulated gel underwent comprehensive evaluation, including assessments for gelation, drug content, in vitro drug release, ex vivo permeation, and histopathology.

Result: The findings demonstrated superior drug release from the In Situ gel compared to standalone chrysin. Ex vivo studies revealed effective drug permeation through nasal mucosa without causing harm. Moreover, experiments on neuronal cells exposed to oxidative stress (H₂O₂- induced) showcased significant neuroprotection conferred by chrysin and its formulations. These treatments exhibited notable enhancements in cell viability and reduced instances of apoptosis and necrosis, compared to the control group. The formulations exhibited neuroprotective properties by mitigating oxidative damage through mechanisms, like free radical scavenging and restoration of antioxidant enzyme activity.

Conclusion: In conclusion, this developed In situ gel formulation presents a promising novel nasal delivery system for PD therapy. By addressing challenges related to drug properties and administration route, it holds the potential to enhance treatment outcomes and improve the quality of life for individuals with Parkinson's disease.

Background: Mometasone Furoate (MF) is a corticosteroid (glucocorticoid) used to treat eczema, psoriasis, allergies, and rash on the skin; also used to reduce itching, redness, and swelling (inflammation). It has been reported that the bioavailability of MF is less than 11% when given via the nasal route. Encapsulating the drug in niosomes can improve the active pharmaceutical ingredient's bioavailability by enhancing both physical and biological stability.

Objective: The goal of the study is to develop, a non-ionic surfactant-based vesicular system, by loading mometasone furoate, and introducing it into a gel-based formulation by utilizing an appropriate gelling agent, and performing its evaluation.

Methods: The niosome vesicle was prepared by vacuum rotary evaporation method (Thin film hydration method). Gel was prepared using the dispersion method and in-vitro drug diffusion studies using Franz-diffusion cells.

Results: According to the results of the experiments conducted for the study, Mometasone Furoate niosomal gel was prepared utilizing Mometasone Furoate niosomes that were made using the thin film hydration process, Cholesterol, and Span 60, and loaded in various amounts of Carbopol as a geling agent. The niosomes' zeta potential was found to be -24 mV, showing that the formulation is stable. The polydispersity index (PDI) was found to be 0.409 and the average size of niosomes to be 252.7 nm. The performance of the gel of the optimized formulations containing 2% Carbopol showed in vitro diffusion for 7 hours and an increased flux rate as compared to the plain MF.

Conclusion: The experiments carried out during the study led to the conclusion that the thin-film hydration method was suitable for the formation of the MF-niosomes by using Span 60 and Cholesterol (2:1). The gel formulation containing 2% Carbopol indicated better in vitro diffusion following the Higuchi model across all niosomal gel formulations. Niosomal gel can be regarded as the best vesicular carrier for the efficient distribution of mometasone furoate via the transdermal route.

A wide variety of dosage forms are used for the oral administration of drugs to humans and animals. Apart from solid dosage forms, it also includes liquid dosage forms, such as solutions, suspensions, and emulsions. The selection is based on the physiochemical attributes of the therapeutically active ingredient. Suspensions are classified as dispersed systems that are heterogeneous in nature and consist of two phases. One phase is the continuous phase, the dispersion medium, or the external phase, which is either liquid or semisolid; the other is a solid particle dispersed in the external phase and called an internal or dispersed phase. They have several advantages over other dosage forms, such as effectively delivering hydrophobic drugs, avoiding the need for cosolvents, masking unpleasant tastes, and providing resistance to degradation and easy swallowing for young or elderly patients. They also attain higher drug concentrations compared to solution forms. This review article aims to study and explore the advantages, novel suspending agents, patent preference, and innovations of pharmaceutical suspension. It was targeted to scrutinize the literature floating in the internet domain regarding pharmaceutical suspension for delivery of drugs by oral route. The literature survey is targeted at the novel herbal suspending agents used, their patents involved, and innovations in the dosage form. Further, the study gives an insight into various aspects of suspension, such as classification of suspension, theories of suspension, various components used in suspension formulation, formulation aspect of suspension, evaluation parameters of suspension, patents, innovations, and regulatory status.

Colorectal disease is the third most prevelant cancer in both men and women, with an expected 106,180 new cases of colon cancer and 44,850 new cases of rectal cancer as per American Cancer Society. Targeted medicine delivery is vital in the treatment of colon disorders because it delivers long-term therapeutic results with little side effects. Natural polymer is biocompatible and biodegradable, which enables safety, improves storage, and physiological stability, it is utilized as drug delivery vehicles and has made great strides in recent years. Chitosan, alginate, pectin, guar gum, dextran, hyaluronic acid, and arabinoxylan are examples of natural polysaccharides that are utilized to create nanoparticles. Natural gums serve two purposes: first, they shield the medicine from stomach and intestinal conditions, allowing it to only be released in the colon. In this review, we introduce the different gum particularly used in nanoparticles formulation, and then discuss recent research and the latest patent in the development of gum-based nanoparticles for the treatment of colon rectal cancer.

The development of Monoclonal antibodies (mAbs) has also allowed researchers to understand the complexity of diseases better and find new treatments for difficult-to-treat conditions. Using mAbs, researchers can identify and target specific molecules in the body involved in the disease process. This has allowed for a more targeted treatment approach, which has resulted in improved outcomes for many patients. This hypothesis has been the basis for the development of mAbs that can target an array of illnesses. In the past two decades, therapeutic mAbs have been developed to treat cancer, autoimmune diseases, cardiovascular diseases, and metabolic diseases. For instance, using mAbs has improved outcomes in treating rheumatoid arthritis, multiple sclerosis, and Crohn's disease. However, delivering mAbs in biological systems remains a significant challenge in drug delivery. This is due to their large size, low stability in circulation, and difficulties in achieving their desired action in the target cells. Monoclonal antibodies (mAbs) are an essential tool in biological systems, as they can be used to deliver drugs to specific cell types or tissues. Cloning methods of monoclonal antibody production have been developed to produce mAbs with therapeutic potential. Hence, the present review focused on the development and drug delivery of Monoclonal antibodies (mAbs) in biological systems, which includes cloning methods, various drug delivery technologies, formulation production technology, and its applications in multiple diseases were focused for this review.

Background: The topical drug delivery system has gained more attention in recent years as compared to oral and parenteral drug delivery. However, owing to the barrier function of the skin's topmost layer, only a few drug molecules can be administered by this route. Therefore, encapsulating the drugs in glycerosomes is one potential solution to this problem. Glycerosomes are vesicular drug delivery systems primarily made up of large concentrations of glycerol, phospholipid, water, and other active ingredients.

Objective: The main aim of this review is to summarize the most recent information on the encapsulated vesicular system used in cosmetic preparations, specifically glycerosomes made from both synthetic and naturally occurring plant bioactive substances.

Purpose: Glycerosomes offer many benefits, including increased efficacy, better stability, improve absorption, drug targeting at specific sites, and delivering the same at a predetermined rate.

Method: The mechanism behind the penetration of glycerosomes is the hydration and lipid fluidization of skin, fabricated by glycerol.

Result: Numerous methods have been reported for the formulation of glycerosomes, including the thin film hydration method, reverse-phase evaporation, solvent spherule, detergent removal method, and so on.

Conclusion: Researchers are currently investigating the potential of glycerosomes as nanocarriers for natural bioactive and synthetic drugs. This review describes the structure of glycerosomes, preparation techniques, applications, distinctions from liposomes, and benefits of glycerosomes.

Background: Cystic fibrosis is the predominant autosomal recessive disorder known to reduce life expectancy. Research findings indicate that around 60 to 70% of adult individuals with this condition carry infections of Pseudomonas aeruginosa.

Objective: The ongoing research investigates the potential synergy of merging ivacaftor and ciprofloxacin to address bacterial infections.

Methods: The two drugs were spray-dried into microparticles, which were then coated with Lsalbutamol and were to be delivered by a dry powder inhaler. Microparticles were generated by applying the spray drying method, utilizing bovine serum albumin and L-leucine in their preparation. Additionally, L-salbutamol was mixed and adsorbed onto the surface of the spray-dried microparticles, and it acted as a bronchodilator.

Results: The microparticles produced via spray drying exhibited a particle size measuring 1.6 ± 0.04 μm, along with a polydispersity ratio of 0.33. Their zeta potential measured -27.3 ± 1.1 mV, while the mass median aerodynamic diameter of these microparticles was 3.74 ± 0.08 μm. SEM, XRD, and FTIR studies confirmed the entrapment of ivacaftor and ciprofloxacin. The morphology was observed by SEM and TEM scans. Antibacterial synergy was confirmed through the agar broth and dilution method, and the formulation's safety was established based on the outcomes of the MTT assay.

Conclusion: Using spray-dried microparticles containing ciprofloxacin, ivacaftor, and L-salbutamol presents a novel approach to the treatment of cystic fibrosis.

Objective: The purpose of this research was to optimize the design and construction of nanoparticle gel (TFN-NPs) loaded with tofacitinib citrate (TFN) using poly lactic co glycolic acid (PLGA).

Method: PLGA (A) as the polymer, polyvinyl alcohol (PVA) (B) as the stabilizer and stirring speed (C) as independent variables were used. TFN-NPs were prepared using single emulsion-solvent evaporation. Box Behnken Design (BBD) was used to determine the optimal component ratio of TFN-NPs based on point prediction.

Results: The entrapment efficiency, particle size, and cumulative drug release of the best-composed TFN-NPs were, respectively, 79.82±0.9%, 236.19±5.07 nm, and 82.31±1.23%; the PDI, zeta potential, and drug loading were, respectively, 0.297±0.21, -30.21±0.94mV, and 69.81±0.16%. Gel formulation employing Carbopol as a gelling polymer was then developed using the optimal TFN-NPs mixture. Gel characterization, drug release, permeation studies, irritation, and pharmacokinetic studies were also conducted. Further solid state and morphology were evaluated using FTIR, DSC, XRD, SEM, TEM, and AFM on the developed topical gel formulation (TFN-NPG) and TFN-NPs. The release and permeation investigations indicated that TFN was slowly released (38.42±2.87%) and had significantly enhanced penetration into the epidermal membrane of mice. The cumulative irritation score of 0.33 determined during testing suggested little discomfort. The generated nanogels are stable and have a high drug penetration profile over the skin, as shown by the findings. When compared to both pure TFN solutions, TFN-NPs and TFN-NPG demonstrated superior pharmacokinetic properties.

Conclusion: Based on the results, the NPs and NPG formulations were depicted to enhance the activity of TFN compared to the free drug solution. TFN could be a safe and effective treatment for Alopecia areata. The tofacitinib citrate NPG could be a clinically translatable, safer topical formulation for managing Alopecia areata.

Background: The main objective of the current research work is to improve the absorption of Nitrofurantoin (NFT) by minimizing gastrointestinal (GI) intolerance and variations in its absorption by formulating the drug into a nanoemulsion (NE).

Method: Based on the highest saturation solubility of NFT, soybean oil, transcutol HP, and labrafil M1944CS were selected as oil, co-surfactant, and surfactant, and a S_mix ratio of 1:2 was selected based on pseudoternary phase diagrams. The formulation prepared with an equal ratio of oil and S_mix exhibited the lowest globule size, highest zeta potential, and higher drug release and hence was selected for further evaluation.

Result: Optimized formulation (NF5) showed improved membrane permeability against pure drug suspension (2.30 times) and marketed suspension formulation (1.43 times). NF5 exhibited similar % cell viability and % cell toxicity in Caco-2 cell lines compared to the marketed suspension. The relative bioavailability of NFT-NE was enhanced by 1.10 and 1.17 times compared to the marketed and pure drug suspension, respectively.

Conclusion: Thus, it can be concluded that the optimized nanoemulsion formulation of NFT exhibited improved membrane permeability, comparable cell viability, and increased relative bioavailability. These findings suggest the potential of the nanoemulsion approach as a strategy to overcome the variability of oral absorption and GI intolerance of NFT.